{"product_id":"m13950","title":"SIAIS178","description":"\u003cp style=\"padding-left: 1em;\"\u003eSIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 2376047-73-1\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 1012.68\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C50H62ClN11O6S2\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e N-(2-chloro-6-methylphenyl)-2-({6-[4-(7-{[(2S)-1-[(2S,4R)-4-hydroxy-2-({[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}carbamoyl)pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl}heptanoyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e CC1N=CSC=1C1=CC=C(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCC(=O)N2CCN(CC2)C2C=C(NC3=NC=C(S3)C(=O)NC3C(Cl)=CC=CC=3C)N=C(C)N=2)C(C)(C)C)C=C1\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e YGQREOJIRFCRKQ-ZIBKGDFVSA-N\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e InChI=1S\/C50H62ClN11O6S2\/c1-30-12-11-13-36(51)43(30)59-47(67)38-27-53-49(70-38)57-39-25-40(56-32(3)55-39)60-20-22-61(23-21-60)42(65)15-10-8-7-9-14-41(64)58-45(50(4,5)6)48(68)62-28-35(63)24-37(62)46(66)52-26-33-16-18-34(19-17-33)44-31(2)54-29-69-44\/h11-13,16-19,25,27,29,35,37,45,63H,7-10,14-15,20-24,26,28H2,1-6H3,(H,52,66)(H,58,64)(H,59,67)(H,53,55,56,57)\/t35-,37+,45-\/m1\/s1\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eTechnical Data\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eAppearance:\u003c\/strong\u003e Solid Power\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003ePurity:\u003c\/strong\u003e ≥98% (or refer to the Certificate of Analysis)\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eSolubility:\u003c\/strong\u003e DMSO : 300 mg\/mL (296.24 mM; Need ultrasonic).\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eShipping Condition:\u003c\/strong\u003e Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eStorage Condition:\u003c\/strong\u003e Dry, dark and -20 \u003csup\u003eo\u003c\/sup\u003eC for 1 year or refer to the Certificate of Analysis.\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eShelf Life:\u003c\/strong\u003e ≥12 months if stored properly.\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eStock Solution Storage:\u003c\/strong\u003e 0 - 4 \u003csup\u003eo\u003c\/sup\u003eC for 1 month or refer to the Certificate of Analysis.\u003c\/p\u003e\n\u003cp style=\"text-indent: -1em; padding-left: 1em;\"\u003e\u003cstrong\u003eDrug Formulation:\u003c\/strong\u003e To be determined\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eHS Tariff Code:\u003c\/strong\u003e 382200\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eHow to use\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eIn Vitro:\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp style=\"padding-left: 1em;\"\u003eSIAIS178 (1-100 nM; for 16 hours) significantly reduces the BCR-ABL protein levels in a concentration dependent manner. SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5. SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity in BCR-ABL driven CML cell lines. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines.\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eIn Vivo:\u003c\/strong\u003e\u003c\/p\u003e\n\u003cp style=\"padding-left: 1em;\"\u003eSIAIS178 (ip; 5, 15, and 45 mg\/kg; 12 days) attenuates tumor progression in a dose-dependent manner, as determined by serial volumetric measurement . SIAIS178 (iv or ip; 2 mg\/kg; 24 hours) has T1\/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively.\u003c\/p\u003e\n\u003cp\u003e\u003cstrong\u003eProducts are for research use only. Not for human use.\u003c\/strong\u003e\u003c\/p\u003e","brand":"Xcess Biosciences","offers":[{"title":"M13950-2 \/ Contact sales@xcessbio.com for quotation","offer_id":39462371197067,"sku":"","price":100.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0389\/1897\/9723\/files\/1686549108477.png?v=1686549128","url":"https:\/\/www.xcessbio.com\/products\/m13950","provider":"Xcess Biosciences","version":"1.0","type":"link"}